6. • Drug Class: ANTIBIOTIC.
• Structure:
• Main structural activity: 7-aminocephalosporanic acid.
R1 and R2 are the sites of potential
biochemical manipulation.
7. Drug’s Name Cefazolin Cefaclor Ceftriaxone Cefipime
Chemical Beta lactams --------- --------- ---------
Pharmacological Cephalosporin
(1ST generation)
(2ND generation) (3RD generation) (4TH generation
Therapeutic antibiotics
--------- --------- ---------
Drug Class
8. • They are Bactericidal and has the mode of action as other beta-lactam
antibiotics.
The b-lactam antibiotics inhibit the last step in peptidoglycan synthesis,
presumably by acylating the transpeptidase via cleavage of the—CO—N—bond of the
b-lactam ring.
The transpeptidase responsible for peptidoglycan synthesis
also known as Penicilin binding protein PBPs.
Mechanism Of Action
9.
10. Drugs SPECTRUM
CEFAZOLINE Good activity against gram-positive bacteria and relatively modest activity against
gram-negative microorganisms
Staphylococcus
CEFACLOR Extended Gram Negative coverage
Haemophilus influenzae
Moraxella catarrhalis
CEFTRIAXONE Less active than first-generation agents against gram-positive cocci but are much
more active against
Haemophilus influenzae
penicillin-sensitive S. pneumoniae
Neisseria meningitides
gonorrhea
CEFEPIME Extended activity spectrum compared with the third generation
Pseudomonas.aeruginosa
Haemophilus influenzae,
Neisseria gonorrhoeae
Neisseria meningitides
Enterobacteriaceae
11. DRUGS CEFAZOLINE CEFACLOR CEFTRIAXONE CEFEPIME
INDICATIONS • Severe infection
• Prophylaxis of
infections during
surgery
• Endocarditis
•Infections
URT
LRT
UTI
Skin
•Bronchitis
•Pharyngitis
•Severe infections
•Surgical prophylaxis
•Uncomplicated
gonorrhea
•Meningitis
•Pneumonia
•Febrile
neutropenia
• UTI
Indications
12. Pharmacokinetics
Drugs Absorption Distribution Metabolism Elimination
B Vd PPB T1/2
hr
Cl BB
B
Pl
Cefazolin (iv) poor 100 9.21 85 2 80 No yes Liver Unchange in
urine
Cefaclor (oral) well 23ug/
ml
0.37L 25 0.5-1 0.92 mil
d
yes liver In kidney
85% unchanged
in urine
Ceftriaxone(iv,im) complete 100 5-13L 85-
95
6-9 49ml yes yes liver 40-65%
unchanged in
urine
Cefipime (iv) rapid 100 16-20L 20 2 120ml/
min
yes yes Liver N-
methylpyrrolidi
ne (NMP
85 % renal
13.
14. Adverse effects
Similar Different
Git disturbance
Hypersensitivity reactions
(e.g skin rashes, urticaria, eosinophilia, fever,
anaphylaxis)
Cefipime:
• back and legs pain
• bleeding gums, nosebleeds
• confusion, headache
• dark urine , difficulty with breathing.
• numbness and tingling.
• yellowing of the eyes or skin
Ceftriaxone
•Calcium ceftriaxone precipitation in gall
bladder and in urine.
15. Containdications
Conditions Drugs
Hypersensitivity Cefazolin ,cefaclor,ceftriaxone and
cefipime
Penicillin hypersensitivity Cefipime
Concomitant treatment with
calcium (TPN)
(risk of precipitation inurine and
lungs in neonates )
Ceftriaxone:
Pregnancy category (B)
Excreted in milk Yes (continue)
16. Precautions
CEFAZOLINE CEFACLOR CEFTRIAXONE CEFEPIME
• Use with caution
in renal
dysfunction.
• Avoid in patients
with aspirin
hypersensitivity.
• Avoid if patient
has allergic history.
• It can give false
positive coombs*
test .
• It cause ppt. In
gall bladder.
• It may displace
serum albumin.
• Use with caution
in renal
dysfunction.
• Avoid if patient
has allergic history.
*The Coombs test will help your doctor determine if you have antibodies in your bloodstream that are causing
your immune system to attack and destroy your own red blood cells resulting hemolytic anemia.
